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Titolo:
NK2 receptors mediate tachykinin-induced contractions of rat uterus duringthe oestrous cycle
Autore:
Moodley, N; Lau, WAK; Pennefather, JN; Story, ME; Fisher, L;
Indirizzi:
Monash Univ, Dept Pharmacol, Clayton, Vic 3168, Australia Monash Univ Clayton Vic Australia 3168 acol, Clayton, Vic 3168, Australia
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 1-2, volume: 376, anno: 1999,
pagine: 53 - 60
SICI:
0014-2999(19990702)376:1-2<53:NRMTCO>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
ESTROGEN-PRIMED RAT; ANGIOTENSIN-CONVERTING ENZYME; SUBSTANCE-P; ANTAGONIST; INNERVATION; INHIBITORS; RESPONSES; AFFERENT; POTENT; NERVES;
Keywords:
tachykinin NK2; receptors; non-peptide tachykinin receptor antagonist; uterine contraction; oestrous cycle;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
30
Recensione:
Indirizzi per estratti:
Indirizzo: Pennefather, JN Monash Univ, Dept Pharmacol, Clayton, Vic 3168, Australia Monash Univ Clayton Vic Australia 3168 ic 3168, Australia
Citazione:
N. Moodley et al., "NK2 receptors mediate tachykinin-induced contractions of rat uterus duringthe oestrous cycle", EUR J PHARM, 376(1-2), 1999, pp. 53-60

Abstract

We examined tachykinin-induced contractions of uteri from rats during the oestrous cycle. The potencies of substance P, neurokinin A, neurokinin B and the tachykinin NK2 receptor-selective agonist, [Lys(5), MeLeu(9), Nle(10)] neurokinin A-(4-10), and of the non-peptide tachykinin NK1, NK2 and NK3 receptor antagonists (S)1-{2-[3-(3,4-dichlorophenyl)-1-(3-isopropoxyphenylacetyl)piperidin-3-yl]ethyl}-4-phenyl-1-azonia-bicyclo[2.2.2]octane (SR 140333), (S)-N-methyl-N [4-(4-acetylamino-4-phenylpiperidino)-2-(3,4-dichlorophenyl)butyl]benzamide (SR 48968) and (S)-( N)-(1-(3-(1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl)propyl) N-methylacetamide (SR 142801), were examined. The relative agonist potencies, i.e., [Lys(5), MeLeu(9), Nle(10)] neurokinin A-(4-10) greater than or equal to neurokinin A > neurokinin B greater than or equal to substance P were similar in preparations from rats in dioestrus/metoestrus and those in proestrus/oestrus. Apparent pK(B) values for SR 48968 versus neurokinin A and [Lys(5), MeLeu(9), Nle(10)] neurokinin A-(4-10), were 9.9 and 9.2, respectively, indicating activation of an NK2 receptor. SR 140333 (10 nM) produced only a small rightward shift of the log concentration-response curve to substance P. SR 48968 (3 nM), but not SR 142801 (100-300 nM) reduced the effect of neurokinin B. These data indicate thatin the rat tachykinin-induced contract-ions of the uteri during the oestrous cycle are mediated primarily by tachykinin NK2 receptors, and that fluctuations in ovarian hormonal levels during the oestrous cycle have little influence on the uterine response to tachykinins. (C) 1999 Elsevier Science B. V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/11/20 alle ore 21:32:26